Caspase-8

A caspase-8 that is encoded in the genome of human. [PRO:DNx]

Synonyms

CASP-8;
EC 3.4.22.61;
Apoptotic cysteine protease;
Apoptotic protease Mch-5;
CAP4;
FADD-homologous ICE/ced-3-like protease;
FADD-like ICE;
FLICE;
ICE-like apoptotic protease 5;
MORT1-associated ced-3 homolog;
MACH

Research

Bioassay Publications (10)

Timeframe	Studies on this Protein(%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	8 (80.00)	29.6817
2010's	2 (20.00)	24.3611
2020's	0 (0.00)	2.80

Compounds (16)

Drugs with Inhibition Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
isoquinoline-1,3,4-trione	Homo sapiens (human)	IC50	1.0598	2	6
n-methylisatin	Homo sapiens (human)	IC50	50.0000	1	1
pralnacasan	Homo sapiens (human)	IC50	0.0400	2	2
acetyl-aspartyl-glutamyl-valyl-aspartal	Homo sapiens (human)	IC50	0.0602	5	10
5-Nitroisatin	Homo sapiens (human)	IC50	3.0000	1	1
n-acetyltyrosyl-valyl-alanyl-aspartyl aldehyde	Homo sapiens (human)	IC50	0.0082	2	2
benzyloxycarbonyl-phe-ala-fluormethylketone	Homo sapiens (human)	IC50	100.0000	1	1
benzyloxycarbonylvalyl-alanyl-aspartyl fluoromethyl ketone	Homo sapiens (human)	Ki	0.0180	1	0
grassystatin a	Homo sapiens (human)	IC50	5.0000	1	1

Drugs with Other Measurements

Drug	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Publication(s)
3,3',4,5'-tetrahydroxystilbene	Homo sapiens (human)	AC50	70.0000	1	0
2,2'-((3,3'-dimethoxy(1,1'-biphenyl)-4,4'-diyl)diimino)bis-benzoic acid	Homo sapiens (human)	AC50	47.9700	1	0
stictic acid	Homo sapiens (human)	AC50	70.0000	1	0
1,3(2h,4h)-isoquinolinedione	Homo sapiens (human)	AC50	1.0900	1	0
1,6-dimethyl-3-(2-pyridinyl)pyrimido[5,4-e][1,2,4]triazine-5,7-dione	Homo sapiens (human)	AC50	0.4360	1	0
1,6-dimethyl-3-propylpyrimido[5,4-e][1,2,4]triazine-5,7-dione	Homo sapiens (human)	AC50	0.3100	1	0
MK-8353	Homo sapiens (human)	Activity	0.1850	1	1

Enables

This protein enables 13 target(s):

Target	Category	Definition
cysteine-type endopeptidase activity	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE, https://www.ebi.ac.uk/merops/about/glossary.shtml#ENDOPEPTIDASE]
death receptor binding	molecular function	Binding to a member of the death receptor (DR) family. The DR family falls within the tumor necrosis factor receptor superfamily and is characterized by a cytoplasmic region of ~80 residues termed the death domain (DD). [GOC:ceb, GOC:rl, PMID:15654015]
tumor necrosis factor receptor binding	molecular function	Binding to a tumor necrosis factor receptor. [GOC:ai]
protein binding	molecular function	Binding to a protein. [GOC:go_curators]
peptidase activity	molecular function	Catalysis of the hydrolysis of a peptide bond. A peptide bond is a covalent bond formed when the carbon atom from the carboxyl group of one amino acid shares electrons with the nitrogen atom from the amino group of a second amino acid. [GOC:jl, ISBN:0815332181]
cysteine-type peptidase activity	molecular function	Catalysis of the hydrolysis of peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile. [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE]
ubiquitin protein ligase binding	molecular function	Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp]
death effector domain binding	molecular function	Binding to a DED domain (death effector domain) of a protein, a homotypic protein interaction module composed of a bundle of six alpha-helices that is related in structure to the death domain (DD). [GOC:ecd, InterPro:IPR001875]
identical protein binding	molecular function	Binding to an identical protein or proteins. [GOC:jl]
protein-containing complex binding	molecular function	Binding to a macromolecular complex. [GOC:jl]
scaffold protein binding	molecular function	Binding to a scaffold protein. Scaffold proteins are crucial regulators of many key signaling pathways. Although not strictly defined in function, they are known to interact and/or bind with multiple members of a signaling pathway, tethering them into complexes. [GOC:BHF, GOC:sjp, PMID:10433269, Wikipedia:Scaffold_protein]
cysteine-type endopeptidase activity involved in apoptotic process	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile, and contributing to the apoptotic process. [GOC:mtg_apoptosis]
cysteine-type endopeptidase activity involved in apoptotic signaling pathway	molecular function	Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a mechanism in which the sulfhydryl group of a cysteine residue at the active center acts as a nucleophile, and contributing to the apoptotic signaling pathway. [GOC:mtg_apoptosis, PMID:11717445, Wikipedia:Caspase]

Located In

This protein is located in 7 target(s):

Target	Category	Definition
nucleoplasm	cellular component	That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653]
mitochondrion	cellular component	A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732]
mitochondrial outer membrane	cellular component	The outer, i.e. cytoplasm-facing, lipid bilayer of the mitochondrial envelope. [GOC:ai]
cytosol	cellular component	The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl]
cytoskeleton	cellular component	A cellular structure that forms the internal framework of eukaryotic and prokaryotic cells. The cytoskeleton includes intermediate filaments, microfilaments, microtubules, the microtrabecular lattice, and other structures characterized by a polymeric filamentous nature and long-range order within the cell. The various elements of the cytoskeleton not only serve in the maintenance of cellular shape but also have roles in other cellular functions, including cellular movement, cell division, endocytosis, and movement of organelles. [GOC:mah, PMID:16959967, PMID:27419875]
lamellipodium	cellular component	A thin sheetlike process extended by the leading edge of a migrating cell or extending cell process; contains a dense meshwork of actin filaments. [ISBN:0815316194]
cell body	cellular component	The portion of a cell bearing surface projections such as axons, dendrites, cilia, or flagella that includes the nucleus, but excludes all cell projections. [GOC:go_curators]

Active In

This protein is active in 1 target(s):

Target	Category	Definition
cytoplasm	cellular component	The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684]

Part Of

This protein is part of 4 target(s):

Target	Category	Definition
death-inducing signaling complex	cellular component	A protein complex formed by the association of signaling proteins with a death receptor upon ligand binding. The complex includes procaspases and death domain-containing proteins in addition to the ligand-bound receptor, and may control the activation of caspases 8 and 10. [GOC:mtg_apoptosis, PMID:12628743, PMID:12655293, PMID:8521815]
CD95 death-inducing signaling complex	cellular component	A protein complex formed upon binding of Fas/CD95/APO-1 to its ligand. The complex includes FADD/Mort1, procaspase-8/10 and c-FLIP in addition to the ligand-bound receptor. [PMID:12628743, PMID:12655293]
protein-containing complex	cellular component	A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah]
ripoptosome	cellular component	A protein complex whose core components are the receptor-interacting serine/threonine-protein kinases RIPK1 and RIPK3 (also called RIP1 and RIP3). Formation of the ripoptosome can induce an extrinsic apoptotic signaling pathway or a necroptotic signaling pathway. The composition of this protein complex may depend on several factors including nature of the signal, cell type and more. [GOC:bhm, GOC:mtg_apoptosis, PMID:22265414, PMID:22274400]

Involved In

This protein is involved in 39 target(s):

Target	Category	Definition
angiogenesis	biological process	Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453]
regulation of cytokine production	biological process	Any process that modulates the frequency, rate, or extent of production of a cytokine. [GOC:add, ISBN:0781735149]
proteolysis	biological process	The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah]
apoptotic process	biological process	A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263]
heart development	biological process	The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948]
regulation of tumor necrosis factor-mediated signaling pathway	biological process	Any process that modulates the rate or extent of the tumor necrosis factor-mediated signaling pathway. The tumor necrosis factor-mediated signaling pathway is the series of molecular signals generated as a consequence of tumor necrosis factor binding to a cell surface receptor. [GOC:dph, GOC:tb]
natural killer cell activation	biological process	The change in morphology and behavior of a natural killer cell in response to a cytokine, chemokine, cellular ligand, or soluble factor. [GOC:mgi_curators, ISBN:0781735149]
macrophage differentiation	biological process	The process in which a relatively unspecialized monocyte acquires the specialized features of a macrophage. [GOC:add, ISBN:0781735149]
positive regulation of cell migration	biological process	Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators]
response to cobalt ion	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cobalt ion (Co2+) stimulus. [GOC:mah]
response to estradiol	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of stimulus by estradiol, a C18 steroid hormone hydroxylated at C3 and C17 that acts as a potent estrogen. [GOC:mah, ISBN:0911910123]
response to lipopolysaccharide	biological process	Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464]
positive regulation of interleukin-1 beta production	biological process	Any process that activates or increases the frequency, rate, or extent of interleukin-1 beta production. [GOC:mah]
response to tumor necrosis factor	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a tumor necrosis factor stimulus. [GOC:mah]
TRAIL-activated apoptotic signaling pathway	biological process	An extrinsic apoptotic signaling pathway initiated by the binding of the ligand TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) to a death receptor on the cell surface. [GOC:bf, GOC:PARL, PMID:21785459]
T cell activation	biological process	The change in morphology and behavior of a mature or immature T cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149]
B cell activation	biological process	The change in morphology and behavior of a mature or immature B cell resulting from exposure to a mitogen, cytokine, chemokine, cellular ligand, or an antigen for which it is specific. [GOC:mgi_curators, ISBN:0781735149]
positive regulation of apoptotic process	biological process	Any process that activates or increases the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis]
positive regulation of canonical NF-kappaB signal transduction	biological process	Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
negative regulation of canonical NF-kappaB signal transduction	biological process	Any process that stops, prevents, or reduces the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl]
regulation of innate immune response	biological process	Any process that modulates the frequency, rate or extent of the innate immune response, the organism's first line of defense against infection. [GOC:ebc]
response to ethanol	biological process	Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ethanol stimulus. [GOC:go_curators]
positive regulation of macrophage differentiation	biological process	Any process that activates or increases the frequency, rate or extent of macrophage differentiation. [GOC:go_curators]
positive regulation of proteolysis	biological process	Any process that activates or increases the frequency, rate or extent of the hydrolysis of a peptide bond or bonds within a protein. [GOC:go_curators]
proteolysis involved in protein catabolic process	biological process	The hydrolysis of a peptide bond or bonds within a protein as part of the chemical reactions and pathways resulting in the breakdown of a protein by individual cells. [GOC:ai, GOC:dph, GOC:tb]
protein maturation	biological process	Any process leading to the attainment of the full functional capacity of a protein. [GOC:ai]
negative regulation of necroptotic process	biological process	Any process that decreases the rate, frequency or extent of a necroptotic process, a necrotic cell death process that results from the activation of endogenous cellular processes, such as signaling involving death domain receptors or Toll-like receptors. [GOC:BHF, GOC:dph, GOC:mtg_apoptosis, GOC:tb]
syncytiotrophoblast cell differentiation involved in labyrinthine layer development	biological process	The process in which a chorionic trophoblast cell acquires specialized features of a syncytiotrophoblast of the labyrinthine layer of the placenta. [GOC:dph]
pyroptosis	biological process	A caspase-1-dependent cell death subroutine that is associated with the generation of pyrogenic mediators such as IL-1beta and IL-18. [GOC:mtg_apoptosis, PMID:18846107, PMID:21760595]
cellular response to mechanical stimulus	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a mechanical stimulus. [GOC:mah]
cellular response to organic cyclic compound	biological process	Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an organic cyclic compound stimulus. [GOC:mah]
apoptotic signaling pathway	biological process	The series of molecular signals which triggers the apoptotic death of a cell. The pathway starts with reception of a signal, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis]
extrinsic apoptotic signaling pathway	biological process	The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with either a ligand binding to a cell surface receptor, or a ligand being withdrawn from a cell surface receptor (e.g. in the case of signaling by dependence receptors), and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis, GOC:yaf, PMID:17340152]
execution phase of apoptosis	biological process	A stage of the apoptotic process that starts with the controlled breakdown of the cell through the action of effector caspases or other effector molecules (e.g. cathepsins, calpains etc.). Key steps of the execution phase are rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:mtg_apoptosis, PMID:21760595]
activation of cysteine-type endopeptidase activity	biological process	Any process that initiates the activity of the inactive enzyme cysteine-type endopeptidase. [GOC:mtg_apoptosis, PMID:21726810]
self proteolysis	biological process	The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their own peptide bonds. [GOC:yaf, PMID:18676612, PMID:19144634]
activation of cysteine-type endopeptidase activity involved in apoptotic process	biological process	Any process that initiates the activity of the inactive enzyme cysteine-type endopeptidase in the context of an apoptotic process. [GOC:al, GOC:dph, GOC:jl, GOC:mtg_apoptosis, GOC:tb, PMID:14744432, PMID:18328827, Wikipedia:Caspase]
extrinsic apoptotic signaling pathway via death domain receptors	biological process	The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with a ligand binding to a death domain receptor on the cell surface, and ends when the execution phase of apoptosis is triggered. [GOC:mah, GOC:mtg_apoptosis]
positive regulation of neuron apoptotic process	biological process	Any process that activates or increases the frequency, rate or extent of cell death of neurons by apoptotic process. [GOC:go_curators, GOC:mtg_apoptosis]

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